Abstract

Aurora kinase A (Aurora-A), a member of the Aurora family of serine/threonine kinases, plays a critical role in multiple steps of mitotic progression, including microtubule stability during the G1 phase of the cell cycle, chromosome alignment and segregation, and cytokinesis and is aberrantly expressed in various types of human cancers. In addition to its classic functions, recent studies have indicated that Aurora-A is critical for controlling self-renewal of embryonic stem cells through negative regulation of p53. Additionally, aberrant expression of Aurora-A contributes to oncogenic transformation and induces stem cell-like properties in estrogen receptor α-positive breast cancer cells. Silencing of Aurora-A has been implicated in elimination of leukemia stem cells in vivo. Therefore, Aurora-A is an attractive target for cancer therapeutics and a growing number of small molecule inhibitors of Aurora-A have been developed. In the present review, we will address the role of Aurora-A in cancer stem cells, as well as the outcomes of clinical trials assessing Aurora-A-specific small molecular inhibitors.

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